Dorsomorphin (Compound C)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Dorsomorphin是细胞渗透性的\可逆的和ATP竞争性的AMP激活蛋白激酶(AMPK)抑制剂,Ki值为109 nM[1].
相较其他结构相关的激酶,如蛋白激酶A\蛋白激酶C和Janus激酶3,dorsomorphin对AMPK具有高选择性.在葡萄糖剥夺的小鼠神经干细胞中,dorsomorphin作为AMPK抑制剂,被发现可逆地抑制AMPK信号通路诱导的抗增殖.在小鼠3T3-L1成纤维细胞中,dorsomorphin显示出成脂分化的抑制作用[2].
Dorsomorphin也被报道是BMP信号通路的抑制剂.它能抑制Smad 1 / 5 / 8的磷酸化作用,从而减少异位骨化.也可以降低肝脏hepcidin的基因转录,随后导致铁水平升高.此外,dorsomorphin对BMP的抑制作用促进人ESC的自我更新和神经诱导[2].
参考文献：
[1] Lu Y, Akinwumi BC, Shao Z, Anderson HD. Ligand Activation of Cannabinoid Receptors Attenuates Hypertrophy of Neonatal Rat Cardiomyocytes. J Cardiovasc Pharmacol. 2014 Jun 26.
[2] Kudo T, Kanetaka H, Mizuno K, et al. Effects of the Small Molecule Dorsomorphin on Intracellular Signaling. Interface Oral Health Science 2011. Springer Japan, 2012: 131-133.
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 399.49 |
| Cas No. | 866405-64-3 |
| Formula | C24H25N5O |
| Synonyms | Compound C |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥8.49 mg/mL in DMSO with gentle warming and ultrasonic |
| Chemical Name | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine |
| SDF | Download SDF |
| Canonical SMILES | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
HT-29人结肠癌细胞和HeLa细胞，斑马鱼胚胎 |
|
溶解方法 |
该化合物可溶于DMSO。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
|
反应条件 |
40 μM，4-10 μM，30 min |
|
应用 |
Dorsomorphin抑制完整肝细胞中的AMPK活性。Dorsomorphin抑制自噬蛋白水解。Dorsomorphin抑制80％ACC磷酸化。Dorsomorphin抑制HT-29细胞中的蛋白水解。在表达LKB1和STRAD的HeLa细胞和对照HeLa细胞中，Dorsomorphin抑制AMPK活性。Dorsomorphin在斑马鱼胚胎中诱导背皮化。Dorsomorphin抑制BMP4诱导的BMP反应性SMAD的磷酸化，IC50为0.47 μM。 |
| 动物实验 [2]: | |
|
动物模型 |
通过尾静脉注射0.2 g/kg葡聚糖的C57BL/6小鼠或0.2 g/kg铁-葡聚糖USP的斑马鱼 |
|
给药剂量 |
腹腔注射，10 mg/kg |
|
应用 |
Dorsomorphin将肝铁调素mRNA水平降低至对照小鼠的三分之一。Dorsomorphin给药24小时以上导致总血清铁浓度增加60％。在小鼠中注射dorsomorphin消除了铁介导的肝SMAD1/5/8磷酸化增加。在成年斑马鱼中，腹腔注射铁-葡聚糖1小时内，肝脏提取物中SMAD1/5/8磷酸化几乎增加三倍。与注射铁葡聚糖和对照组的斑马鱼相比，铁-葡聚糖和dorsomorphin联合使用使SMAD1/5/8磷酸化水平降低近3倍。 |
|
注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
|
References: [1]. Meley D, Bauvy C, Houben-Weerts J H P M, et al. AMP-activated protein kinase and the regulation of autophagic proteolysis[J]. Journal of biological chemistry, 2006, 281(46): 34870-34879. [2]. Paul B Y, Hong C C, Sachidanandan C, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism[J]. Nature chemical biology, 2008, 4(1): 33-41. |
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质量控制和MSDS
- 批次:
化学结构
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